| Identification | Back Directory | [Name]
MK 0343 | [CAS]
233275-76-8 | [Synonyms]
MK 0343
MRK-409
MK-0343 >=98% (HPLC)
7-Cyclobutyl-3-(2,6-difluorophenyl)-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-1,2,4-triazo[4,3-b]pyridazine
7-Cyclobutyl-3-(2,6-difluorophenyl)-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-1,2,4-triazolo[4,3-b]pyridazine
1,2,4-Triazolo[4,3-b]pyridazine, 7-cyclobutyl-3-(2,6-difluorophenyl)-6-[(1-Methyl-1H-1,2,4-triazol-5-yl)Methoxy]- | [Molecular Formula]
C19H17F2N7O | [MDL Number]
MFCD22683821 | [MOL File]
233275-76-8.mol | [Molecular Weight]
397.38 |
| Chemical Properties | Back Directory | [density ]
1.57±0.1 g/cm3(Predicted) | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
DMSO: soluble10mg/mL, clear | [form ]
powder | [pka]
2.11±0.10(Predicted) | [color ]
white to beige | [InChI]
1S/C19H17F2N7O/c1-27-16(22-10-23-27)9-29-19-12(11-4-2-5-11)8-15-24-25-18(28(15)26-19)17-13(20)6-3-7-14(17)21/h3,6-8,10-11H,2,4-5,9H2,1H3 | [InChIKey]
GOIFCXRIFSYPFG-UHFFFAOYSA-N | [SMILES]
Cn1ncnc1COc2nn3c(nnc3cc2C4CCC4)-c5c(F)cccc5F |
| Hazard Information | Back Directory | [Uses]
MK 0343 is a subtype-selective partial GABAA receptor agonist with the ability to cause anxiolytic and non-sedating properties. | [Biological Activity]
MK-0343 (MRK-409) is a partial agonist for GABAA receptors with comparable Ki values for α1α2α3 and α5 containing receptors (0.2 – 0.4 nM). The compound has the greatest agonist activity against α3 receptorsand is brain penatrantand displays anxiolytic activity in rodent and primate models. | [in vivo]
MK0343 readily penetrates the brain in rats and occupies the benzodiazepine site of GABAA receptors, measured using an in vivo [3H]flumazenil binding assay, with an Occ50 of 2.2 mg/kg p.o. and a corresponding plasma EC50 of 115 ng/mL[1].
| Animal Model: | Male Sprague-Dawley rats (approximately 250–300g) (pharmacokinetics)[1] | | Dosage: | 1, 2 or 3?mg/kg | | Administration: | Oral administration | | Result: | Readily penetrated the brain in rats and occupies the benzodiazepine site of GABAA receptors, with an Occ50 of 2.2?mg/kg p.o. and a corresponding plasma EC50 of 115?ng/mL. |
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| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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